Ginkgolide B

tert-butyl 6,10-dihydroxy-3,9-dimethyl-4,14-dioxo-15-oxapentacyclo[11.3.1.02,11.05,10.07,11]heptadec-13-ene-8-carboxylate

Chemical Class

Diterpene Trilactone

Molecular Formula

C20H24O10

Molecular Weight

424.4 g/mol

Half-Life

Plasma half-life approximately 4–6 hours. Biliary excretion contributes to enterohepatic recirculation. Renal elimination is the primary route of clearance.

Bioavailability

Moderate oral bioavailability (~30%). Rapidly absorbed with peak plasma levels within 1–2 hours. Crosses the blood-brain barrier. Eliminated primarily via renal excretion.

Known Effects

Potent platelet-activating factor (PAF) receptor antagonist. Neuroprotective, anti-inflammatory, anti-allergic, and bronchodilatory activity. Key compound in standardised ginkgo extracts for cerebrovascular and peripheral vascular applications.

Mechanism of Action

Selective and potent antagonist of the platelet-activating factor (PAF) receptor, inhibiting PAF-induced platelet aggregation, inflammation, and bronchoconstriction. Inhibits neutrophil degranulation and superoxide production. Neuroprotective effects via reduction of excitotoxicity and modulation of neurotransmitter release.

PAF receptorNeutrophil degranulationNF-κB

Safety Data

Well-tolerated at therapeutic doses. Primary safety concern is bleeding due to antiplatelet effects. Contraindicated with anticoagulant therapy. Ginkgolic acids (not ginkgolides) are responsible for allergenic and toxic effects; standardised extracts limit ginkgolic acid content to <5 ppm.

Plant Sources